Aeterna Zentaris Presents Preclinical Data for Its Anti-Cancer PI3K/ Erk 1/2 Inhibitor, AEZS-136, at AACR Meeting
AEZS-136 shows synergy and efficacy in human tumor cells
QUÃ‰BEC CITY, April 3, 2012 /PRNewswire/ – Aeterna Zentaris Inc. (NASDAQ:
AEZS) (TSX: AEZ) (the ”Company”) today announced that a poster on its
novel orally active anticancer PI3K/Erk 1/2 inhibitor, AEZS-136, showed
the compound’s unique inhibition and excellent activity against PI3K
and Erk signaling pathways, as well as being well tolerated. The poster
titled, “Dual inhibition of PI3K and Erk1/2 shows synergy and efficacy in human
tumor cells, either by using drug combinations or novel dual PI3K/Erk
inhibitors“, I. Seipelt, M. Gerlach, L. Blumenstein, G. Mueller, E. Guenther, J.
Engel and M. Teifel, was presented by Irene Seipelt, PhD, Director, Preclinical Development
at Aeterna Zentaris, at the American Association for Cancer Research
Annual Meeting currently held in Chicago.
The anti-proliferative efficacy of AEZS-136 was evaluated in more than
40 human tumor cell lines including breast, ovary, endometrium,
multiple myeloma, lung, melanoma, colon, leukemia and prostate cancer
cells. In vitro ADMET properties were also widely assessed, while in vivo pharmacokinetics (PK) and anti-tumor efficacy was explored. AEZS-136
was well tolerated and showed dose-dependent inhibition of human colon
tumor growth of up to 72% in a Hct116 mouse model.
-- Effective dual targeting of Raf-Mek-Erk and PI3K-Akt pathway -- Unique inhibitor with excellent activity against PI3K and Erk -- Induction of G1 arrest and apoptosis -- Broad anti-proliferative activity in vitro -- Favorable in vitro ADMET and in vivo PK profile -- Well tolerated up to daily doses of 90mg/kg for 4 weeks -- In vivo anti-tumor efficacy after oral administration
Juergen Engel, Ph.D., Aeterna Zentaris’ President and CEO, commented,
“The preclinical data presented yesterday, confirms that AEZS-136 has a
unique advantageous dual PI3K /Erk kinase inhibition profile which
could prove to be more efficient than single pathway inhibition.
Furthermore, AEZS-136 has shown to be well tolerated. Following these
encouraging preclinical data, we are currently moving this promising
compound into the clinical development stage.”
To consult a copy of the poster, please click here.
AEZS-136 is an integral part of the Company’s kinase research program
comprising the investigation of different compounds for single Erk
inhibition, single PI3K inhibition and dual Erk/PI3K kinase inhibition.
AEZS-136 selectively inhibits the kinase activity of Erk 1/2 and class
1 PI3Ks, enabling simultaneous inhibition of the Raf-Mek-Erk and the
PI3K-Akt signaling cascades. AEZS-136 was discovered using our
proprietary compound library and high throughput screening technology.
About Aeterna Zentaris Inc.
Aeterna Zentaris is a late-stage oncology drug development company
currently investigating potential treatments for various cancers. The
Company’s innovative approach of “personalized medicine” means
tailoring treatments to a patient’s specific condition and to unmet
medical needs. Aeterna Zentaris’ deep pipeline is drawn from its
proprietary discovery unit providing the Company with constant and
long-term access to state-of-the-art therapeutic options. For more
information please visit www.aezsinc.com.
This press release contains forward-looking statements made pursuant to
the safe harbour provisions of the U.S. Securities Litigation Reform
Act of 1995. Forward-looking statements involve known and unknown risks
and uncertainties that could cause the Company’s actual results to
differ materially from those in the forward-looking statements. Such
risks and uncertainties include, among others, the availability of
funds and resources to pursue R&D projects, the successful and timely
completion of clinical studies, the risk that safety and efficacy data
from any of our Phase 3 trials may not coincide with the data analyses
from previously reported Phase 1 and/or Phase 2 clinical trials, the
ability of the Company to take advantage of business opportunities in
the pharmaceutical industry, uncertainties related to the regulatory
process and general changes in economic conditions. Investors should
consult the Company’s quarterly and annual filings with the Canadian
and U.S. securities commissions for additional information on risks and
uncertainties relating to forward-looking statements. Investors are
cautioned not to rely on these forward-looking statements. The Company
does not undertake to update these forward-looking statements. We
disclaim any obligation to update any such factors or to publicly
announce the result of any revisions to any of the forward-looking
statements contained herein to reflect future results, events or
developments, unless required to do so by a governmental authority or
by applicable law.
SOURCE AETERNA ZENTARIS INC.